Naslov
Sinteza, antiproliferativna aktivnost i interakcija s DNA novih amino supstituiranih benzimidazo[1, 2-a]kinolina
(Synthesis, antiprolifetaive activity and DNA binding studies of novel amino substituted benzimidazo[1, 2-a]quinokines)

Autori
Perin, Nataša ; Martin Kleiner, Irena ; Nhili, Raja ; Laine, William ; David-Cordonnier, Marie-Hélène ; Vugrek, Oliver ; Karminski-Zamola, Grace ; Kralj, Marijeta ; Hranjec, Marijana

Vrsta, podvrsta i kategorija rada
Sažeci sa skupova, sažetak, znanstveni

Izvornik
XXIII. hrvatski skup kemičara i kemijskih inženjera : knjiga sažetaka = XXIII Croatian Meeting of Chemists and Chemical Engineer : Book of abstracts ; Simpozij Vladimir Prelog = Symposium Vladimir Prelog / Hadžiev, Andrea ; Blažeković, Zdenko - Zagreb : Hrvatsko društvo kemijskih inženjera i tehnologa (HDKI), 2013, 145-145

ISBN
978-953-6894-50-5

Skup
Hrvatski skup kemičara i kemijskih inženjera (23 ; 2013)

Mjesto i datum
Osijek, Hrvatska, 21.04.2013. - 24.04.2013

Vrsta sudjelovanja
Poster

Vrsta recenzije
Domaća recenzija

Ključne riječi
benzimidazo[1; 2-a]kinolini; amino supstituenti; antiproliferativna aktivnost; interakcija s ct-DNA; inhibicija topoizomeraze I i II; fluorescentna mikroskopija
(benzimidazo[1; 2-a]quinolines; amino substituents; antiproliferative activity; inhibition of topoisomerase I and II; fluorescence microscopy)

Sažetak
The permanent and growing interest in the synthesis of azino fused benzimidazole derivatives, as a one of the most extensively studied classes of heterocyclic compounds, is a direct consequence of their diverse biological properties. We represent the synthesis of benzimidazo[1, 2-a]quinolines with amino side chains placed on quinoline nuclei in view of our continuing search and finding of new lead structures with chemotherapeutic activities.[1, 2] Amino-substituted compounds were synthesized by uncatalyzed microwave assisted amination from chloro-substituted precursor. All compounds showed prominent antiproliferative activity, while the length of the amino chains linked to the benzimidazo[1, 2-a]quinoline nuclei manipulated the antiproliferative activity. Although the majority of compounds were active in the submircomolar IC50 concentrations, we performed a series of additional experiments to shed more light on the mechanisms of action of the most active ones, including DNA binding, topoisomerases I and II inhibition, cell cycle perturbances and cellular localization.

Izvorni jezik
Engleski

Znanstvena područja
Kemija, Temeljne medicinske znanosti

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